Simple and Efficient Access to N-Tosyl β-Amino Ketones and Their Conversion into 2,4-Disubstituted Azetidines
摘要:
Treatment of N-tosylaldimines with acetophenone at room temperature in the presence of Bf(3)center dot OEt2 as a catalyst furnished the corresponding N-tosyl beta-amino ketones in high yields (77-86%) within 6-9 h. Subsequent reduction and cyclization of these compounds afforded 2,4-disubstituted N-tosylazetidines, comprising a three-step, high-yielding synthesis starting from aldimines.
Treatment of N-tosylaldimines with acetophenone at room temperature in the presence of Bf(3)center dot OEt2 as a catalyst furnished the corresponding N-tosyl beta-amino ketones in high yields (77-86%) within 6-9 h. Subsequent reduction and cyclization of these compounds afforded 2,4-disubstituted N-tosylazetidines, comprising a three-step, high-yielding synthesis starting from aldimines.